Determinants of retinoid X receptor transcriptional antagonism

…, PD Hobbs, VJ Peterson, AA Bhattacharya…

Index: Cavasotto, Claudio N.; Liu, Gang; James, Sharon Y.; Hobbs, Peter D.; Peterson, Valerie J.; Bhattacharya, Ananyo A.; Kolluri, Siva K.; Zhang, Xiao-Kun; Leid, Mark; Abagyan, Ruben; Liddington, Robert C.; Dawson, Marcia I. Journal of Medicinal Chemistry, 2004 , vol. 47, # 18 p. 4360 - 4372

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Citation Number: 37

Abstract

The synthesis and bioactivity of the retinoid X receptor (RXR) antagonist 4-[(3'-n-butyl-5', 6', 7', 8'-tetrahydro-5', 5', 8', 8'-tetramethyl-2'-naphthalenyl)(cyclopropylidene) methyl] benzoic acid and several heteroatom-substituted analogues are described. Ligand design was based on the scaffold of the 3'-methyl RXR-selective agonist analogue and reports that 3'-n- propyl and longer n-alkyl groups conferred RXR antagonism. The transcriptional ...